Bezu, W/Mariam Kibrnesh (2013) In vivo Antimalarial Evaluation of Embelin and some SemiSynthetic Aromatic Amine Substituted Embelin Derivatives from the Fruit of Embelia schimperia. Masters thesis, Addis Ababa University.
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Abstract
Malaria is a major public health problem mainly due to the development of drug resistance by the most lethal causative parasitic species. New drugs with unique structures and mechanism of action are urgently required to treat sensitive and drug-resistant strains of malaria. Historically, compounds containing novel structure from natural origin represent a major source for the discovery and development of new drugs for several diseases. The present study aimed at isolating embelin from the fruit of Embelia schimperia, preparing some semi-synthesized compounds starting from embelin and evaluating of their in vivo antimalarial activities against mice infected with Plasmodium berghei using a 4-days suppressive test. Three novel aromatic substituted embelin derivatives were semisynthesized in good yields (>98%) by using one-step condensation reaction. Structures for the synthesized compounds were determined using IR, 1H NMR 13C NMR and MS. An attempt has been made in this study to provide some insight on recent semisynthetic approaches to antimalarial drug discovery from natural sources with some structural modification. The target compounds, at a dose of 100-400 mg/kg, suppressed P. berghei parasites by 49- 75% which was significantly different from the negative control group (P<0.05). The study further showed that 5-(o-toluidino)-2-hydroxy-3-undecylcyclohexa-2,5-diene-1,4-dione(1A) possesses maximum antimalarial activity (75% suppression) at a dose of 400mg/kg. The synthesized compounds possess considerable antiplasmodial activities which justify the recent semisynthetic approaches to antimalarial drugs discovered from natural sources. In conclusion, some of the semi-synthesized compounds from embelin could be good candidates for treatment of malaria.
| Item Type: | Thesis (Masters) |
|---|---|
| Uncontrolled Keywords: | Antimalarial activities, aromatic substituted embelin, Embelia schimperia |
| Subjects: | Q Science > QD Chemistry R Medicine > R Medicine (General) R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica |
| Divisions: | Africana |
| Depositing User: | Emmanuel Ndorimana |
| Date Deposited: | 04 Oct 2018 11:57 |
| Last Modified: | 04 Oct 2018 11:59 |
| URI: | http://thesisbank.jhia.ac.ke/id/eprint/6745 |
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